Orally bioavailable Syk inhibitors with activity in a rat PK/PD model
- Authors:
- Publication Date:
- Sponsoring Org.:
- USDOE
- OSTI Identifier:
- 1250393
- Resource Type:
- Publisher's Accepted Manuscript
- Journal Name:
- Bioorganic and Medicinal Chemistry Letters
- Additional Journal Information:
- Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Volume: 25 Journal Issue: 20; Journal ID: ISSN 0960-894X
- Publisher:
- Elsevier
- Country of Publication:
- United Kingdom
- Language:
- English
Citation Formats
Thoma, Gebhard, Veenstra, Siem, Strang, Ross, Blanz, Joachim, Vangrevelinghe, Eric, Berghausen, Jörg, Lee, Christian C., and Zerwes, Hans-Günter. Orally bioavailable Syk inhibitors with activity in a rat PK/PD model. United Kingdom: N. p., 2015.
Web. doi:10.1016/j.bmcl.2015.08.037.
Thoma, Gebhard, Veenstra, Siem, Strang, Ross, Blanz, Joachim, Vangrevelinghe, Eric, Berghausen, Jörg, Lee, Christian C., & Zerwes, Hans-Günter. Orally bioavailable Syk inhibitors with activity in a rat PK/PD model. United Kingdom. https://doi.org/10.1016/j.bmcl.2015.08.037
Thoma, Gebhard, Veenstra, Siem, Strang, Ross, Blanz, Joachim, Vangrevelinghe, Eric, Berghausen, Jörg, Lee, Christian C., and Zerwes, Hans-Günter. Thu .
"Orally bioavailable Syk inhibitors with activity in a rat PK/PD model". United Kingdom. https://doi.org/10.1016/j.bmcl.2015.08.037.
@article{osti_1250393,
title = {Orally bioavailable Syk inhibitors with activity in a rat PK/PD model},
author = {Thoma, Gebhard and Veenstra, Siem and Strang, Ross and Blanz, Joachim and Vangrevelinghe, Eric and Berghausen, Jörg and Lee, Christian C. and Zerwes, Hans-Günter},
abstractNote = {},
doi = {10.1016/j.bmcl.2015.08.037},
journal = {Bioorganic and Medicinal Chemistry Letters},
number = 20,
volume = 25,
place = {United Kingdom},
year = {Thu Oct 01 00:00:00 EDT 2015},
month = {Thu Oct 01 00:00:00 EDT 2015}
}
Free Publicly Available Full Text
Publisher's Version of Record
https://doi.org/10.1016/j.bmcl.2015.08.037
https://doi.org/10.1016/j.bmcl.2015.08.037
Other availability
Cited by: 4 works
Citation information provided by
Web of Science
Web of Science
Save to My Library
You must Sign In or Create an Account in order to save documents to your library.
Works referenced in this record:
The SYK tyrosine kinase: a crucial player in diverse biological functions
journal, May 2010
- Mócsai, Attila; Ruland, Jürgen; Tybulewicz, Victor L. J.
- Nature Reviews Immunology, Vol. 10, Issue 6
Phenyl Carboxamide Analogues as Spleen Tyrosine Kinase (Syk) Inhibitors
journal, February 2014
- Brazeau, Jean-Francois; Rosse, Gerard
- ACS Medicinal Chemistry Letters, Vol. 5, Issue 4
Comprehensive analysis of kinase inhibitor selectivity
journal, October 2011
- Davis, Mindy I.; Hunt, Jeremy P.; Herrgard, Sanna
- Nature Biotechnology, Vol. 29, Issue 11
A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design
journal, March 2015
- Beno, Brett R.; Yeung, Kap-Sun; Bartberger, Michael D.
- Journal of Medicinal Chemistry, Vol. 58, Issue 11
R406, an Orally Available Spleen Tyrosine Kinase Inhibitor Blocks Fc Receptor Signaling and Reduces Immune Complex-Mediated Inflammation
journal, August 2006
- Braselmann, Sylvia; Taylor, Vanessa; Zhao, Haoran
- Journal of Pharmacology and Experimental Therapeutics, Vol. 319, Issue 3
Highly potent aminopyridines as Syk kinase inhibitors
journal, September 2012
- Castillo, Marcos; Forns, Pilar; Erra, Montse
- Bioorganic & Medicinal Chemistry Letters, Vol. 22, Issue 17
Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors
journal, February 2013
- Padilla, Fernando; Bhagirath, Niala; Chen, Shaoqing
- Journal of Medicinal Chemistry, Vol. 56, Issue 4
Overcoming Mutagenicity and Ion Channel Activity: Optimization of Selective Spleen Tyrosine Kinase Inhibitors
journal, February 2015
- Ellis, J. Michael; Altman, Michael D.; Bass, Alan
- Journal of Medicinal Chemistry, Vol. 58, Issue 4
Discovery and Profiling of a Selective and Efficacious Syk Inhibitor
journal, February 2015
- Thoma, Gebhard; Smith, Alexander B.; van Eis, Maurice J.
- Journal of Medicinal Chemistry, Vol. 58, Issue 4
Autoinhibition and adapter function of Syk
journal, November 2009
- Kulathu, Yogesh; Grothe, Gesina; Reth, Michael
- Immunological Reviews, Vol. 232, Issue 1
The tyrosine kinase network regulating mast cell activation
journal, March 2009
- Gilfillan, Alasdair M.; Rivera, Juan
- Immunological Reviews, Vol. 228, Issue 1
Spleen tyrosine kinase inhibitors: a review of the patent literature 2010 – 2013
journal, February 2014
- Norman, Peter
- Expert Opinion on Therapeutic Patents, Vol. 24, Issue 5
Syk inhibitors with high potency in presence of blood
journal, May 2014
- Thoma, Gebhard; Blanz, Joachim; Bühlmayer, Peter
- Bioorganic & Medicinal Chemistry Letters, Vol. 24, Issue 10
Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase
journal, April 2014
- Currie, Kevin S.; Kropf, Jeffrey E.; Lee, Tony
- Journal of Medicinal Chemistry, Vol. 57, Issue 9
Using Ovality to Predict Nonmutagenic, Orally Efficacious Pyridazine Amides as Cell Specific Spleen Tyrosine Kinase Inhibitors
journal, February 2014
- Lucas, Matthew C.; Bhagirath, Niala; Chiao, Eric
- Journal of Medicinal Chemistry, Vol. 57, Issue 6
Specific Inhibition of Spleen Tyrosine Kinase Suppresses Leukocyte Immune Function and Inflammation in Animal Models of Rheumatoid Arthritis
journal, October 2011
- Coffey, Greg; DeGuzman, Francis; Inagaki, Mayuko
- Journal of Pharmacology and Experimental Therapeutics, Vol. 340, Issue 2
Molecular cloning of a porcine gene syk that encodes a 72-kDa protein-tyrosine kinase showing high susceptibility to proteolysis
journal, August 1991
- Taniguchi, T.; Kobayashi, T.; Kondo, J.
- Journal of Biological Chemistry, Vol. 266, Issue 24
Inhibition of Spleen Tyrosine Kinase Attenuates Allergen-Mediated Airway Constriction
journal, December 2013
- Moy, Lily Y.; Jia, Yanlin; Caniga, Michael
- American Journal of Respiratory Cell and Molecular Biology, Vol. 49, Issue 6
Design, synthesis of diaminopyrimidine inhibitors targeting IgE- and IgG-mediated activation of Fc receptor signaling
journal, May 2015
- Argade, Ankush; Bhamidipati, Somasekhar; Li, Hui
- Bioorganic & Medicinal Chemistry Letters, Vol. 25, Issue 10
Syk and pTyr'd: Signaling through the B cell antigen receptor
journal, July 2009
- Geahlen, Robert L.
- Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, Vol. 1793, Issue 7
Aurora at the pole and equator: overlapping functions of Aurora kinases in the mitotic spindle
journal, March 2013
- Hochegger, Helfrid; Hégarat, Nadia; Pereira-Leal, Jose B.
- Open Biology, Vol. 3, Issue 3
Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK)
journal, April 2003
- Cywin, Charles L.; Zhao, Bao-Ping; McNeil, Daniel W.
- Bioorganic & Medicinal Chemistry Letters, Vol. 13, Issue 8
Pyrazine-based Syk kinase inhibitors
journal, April 2012
- Forns, Pilar; Esteve, Cristina; Taboada, Lorena
- Bioorganic & Medicinal Chemistry Letters, Vol. 22, Issue 8
An analysis of the diaminopyrimidine patent estates describing spleen tyrosine kinase inhibitors by Rigel and Portola
journal, November 2010
- Moore, William J.; Richard, David; Thorarensen, Atli
- Expert Opinion on Therapeutic Patents, Vol. 20, Issue 12
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor
journal, August 2011
- Liddle, John; Atkinson, Francis L.; Barker, Michael D.
- Bioorganic & Medicinal Chemistry Letters
Protein tyrosine kinase Syk in mast cell signaling
journal, September 2002
- Siraganian, Reuben P.; Zhang, Juan; Suzuki, Katsuhiro
- Molecular Immunology, Vol. 38, Issue 16-18
A new synthesis of 2,1-benzisothiazoles
journal, October 1975
- Singerman, Gary M.
- Journal of Heterocyclic Chemistry, Vol. 12, Issue 5
Discovery and Development of Spleen Tyrosine Kinase (SYK) Inhibitors
journal, February 2012
- Singh, Rajinder; Masuda, Esteban S.; Payan, Donald G.
- Journal of Medicinal Chemistry, Vol. 55, Issue 8
Rational Design of Highly Selective Spleen Tyrosine Kinase Inhibitors
journal, November 2012
- Lucas, Matthew C.; Goldstein, David M.; Hermann, Johannes C.
- Journal of Medicinal Chemistry, Vol. 55, Issue 23
SLP76 and SLP65: complex regulation of signalling in lymphocytes and beyond
journal, January 2006
- Koretzky, Gary A.; Abtahian, Farhad; Silverman, Michael A.
- Nature Reviews Immunology, Vol. 6, Issue 1
Small-molecule inhibitors of spleen tyrosine kinase as therapeutic agents for immune disorders: will promise meet expectations?
journal, October 2014
- Lucas, Matthew C.; Tan, Seng-Lai
- Future Medicinal Chemistry, Vol. 6, Issue 16
Spleen tyrosine kinase: An Src family of non-receptor kinase has multiple functions and represents a valuable therapeutic target in the treatment of autoimmune and inflammatory diseases
journal, December 2009
- Ghosh, Debjani; Tsokos, George C.
- Autoimmunity, Vol. 43, Issue 1